JPH11228370A - Liquid preparation for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a liquid preparation remarkably reduced in bitterness during and after use of xylitol having anticariogenic action by including xylitol, a specific amount of ethanol and a bitterness-controlling agent. SOLUTION: This liquid preparation comprises (A) 1-30 wt.% xylitol, (B) 2-20 wt.% ethanol, (C) a bitterness-controlling agent and (D) as necessary an antiseptic, a fluoride, a surfactant, an exogenous enzyme, a wetting agent, a sweetening agent, a solvent, etc. Grape fruit oil (i), red pepper extract (ii), etc., can be used as the component C. The component (i) is an essential oil used as a flavoring agent in a food field, etc. The component (ii) is an extract of fruit of Capsicum annuum Linne or its variant. The formulating amount of the component C is preferably 0.0001-10 pts.wt. as oil content in the case of component (i) and preferably 0.005-10 pts.wt. expressed in terms of evaporated solid content in the case of component (ii) based on 100 pts.wt. component B.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an oral liquid preparation such as a mouthwash, and more particularly, to an oral liquid preparation capable of remarkably improving palatability of xylitol as an anti-cariogenic agent.

[0002]

2. Description of the Related Art
For the purpose of preventing caries, oral hygiene products such as mouthwashes,
Fluorides, bactericides, plaque-degrading enzymes, and the like have been added as active ingredients together with the solvent ethanol. Although they have achieved a certain caries preventive effect so far, their use is limited to a certain amount or less from the viewpoint of safety, although they are highly effective.

On the other hand, in recent years, the anti-cariogenic effect of xylitol, a natural sweet material, has been attracting attention mainly in Europe and the United States. And its caries reduction effect has been confirmed.

[0004] However, when xylitol is added to a mouthwash, the operation of rinsing with water and the opportunity to ingest a large amount of food for a long time like foods are rare. In order to exert the effect effectively, it is often blended at a relatively high concentration. However, in mouthwashes containing ethanol, the sweetness of xylitol is similar to that of sugar, so that it is sweet and sticky in the mouth, and at the same time, the unique bitterness of xylitol in the presence of ethanol develops after use, and palatability increases. There is a problem that it is extremely poor.

[0005] With respect to the technology for improving the intense sweetness of polyols such as xylitol blended in oral products, a component selected from acetylated sucrose, quinine hydrochloride, quinine sulfate, caffeine, brucine, etc. is blended to effectively enhance palatability Is known to be improved (Japanese Unexamined Patent Publication No. Hei 8-24535).
No. 0). However, there is no effect on the improvement of bitterness of xylitol, and no technical information for reducing bitterness is disclosed.

Accordingly, an object of the present invention is to provide an oral liquid preparation such as a mouthwash which has a significantly reduced bitterness after use during use of xylitol having an anti-cariogenic effect.

[0007]

Means for Solving the Problems and Embodiments of the Invention The present inventors have made intensive studies in order to achieve the above object, and as a result, contain xylitol and 2 to 20% by weight of ethanol based on the whole composition. In the oral liquid formulation, grapefruit oil, by blending one or more of bitterness modifiers such as capsicum extract, during use, found that an oral liquid formulation with significantly reduced bitterness after use can be obtained, The present invention has been made.

Hereinafter, the present invention will be described in detail. The oral liquid preparation of the present invention is prepared and applied as a mouthwash, liquid dentifrice, mouth freshener, etc., and contains xylitol, ethanol, and a bitterness regulator.

Xylitol used in the present invention is one of sugar alcohols having high safety and can be obtained as commercial products from, for example, Towa Kasei Co., Ltd. and Carta Food Science Co., Ltd. The amount of xylitol is from 1 to 30% (% by weight, hereinafter the same) of the whole composition, more preferably from 2 to 15%, in consideration of the anti-caries properties and the effects of ethanol and the bitterness regulator. If it is less than 1%, the anticariogenic effect is not sufficiently exhibited, and if it is more than 30%, bitterness after use will be felt.

[0010] Ethanol is used in an amount of from 2 to 2 in the total composition.
0%, more preferably 3 to 15%. If it is less than 2%, the stability of the product and the feeling of use such as a refreshing feeling are reduced. If it is more than 20%, inconveniences such as excessive mucous membrane stimulation tend to occur.

As the bitterness regulator, grapefruit oil, pepper extract and the like can be used, and one of these can be used alone or in combination of two or more. The grapefruit oil used in the present invention is an essential oil used as a flavor in the food field and the like. In addition, the pepper extract is Capsicum annuum L.
It is an extract of fruit of inne or its variant (Solanaceae), and an organic solvent such as ethanol is generally used as the extraction solvent. In the present invention, since it is used in combination with ethanol, it is particularly preferable to use ethanol solvent extraction. Commercially available grapefruit oil and capsicum extract can be used. For example, as grapefruit oil, Saneigen FFI Co., Ltd.
Grapefruit essence E-10 or the like can be used.

The mixing ratio of the bitterness modifier used in the present invention is as follows:
If the amount of the bitterness regulator is too small, the effect of improving the bitterness is not sufficient, and if the amount is too large, the effect of improving the bitterness corresponding to the compounding amount cannot be expected. 0.0001
-10 parts by weight, more preferably 0.001-5 parts by weight,
It is particularly preferable to add 0.002 to 1 part by weight. In the case of a pepper extract, 0.005 to 10 parts by weight, more preferably 0.01 to 5 parts by weight, in terms of solid content after evaporation.
It is desirable to add 0.02 to 1 part by weight, particularly preferably 0.02 to 1 part by weight.

[0013] The oral liquid preparation of the present invention usually contains medicinal components and other commonly used components such as fungicides, fluorides, surfactants, and the like, as long as they do not inhibit the bitter taste improving effect on xylitol. Agents, enzymatic agents, wetting agents, sweeteners, preservatives, solvents and the like can be incorporated in usual amounts.

The following are specific examples of medicinal components that can be incorporated into the composition of the present invention. For example, tranexamic acid, antiplasmin agents such as epsilon aminocaproic acid, glycyrrhizin, glycyrrhizinate, anti-inflammatory agents such as allantoin, ascorbate, vitamins such as tocopherol esters, dextranase, mutanase, enzymes such as lysozyme, Crude drug components such as oak extract, gongon extract, clove extract, etc., fluorides such as sodium monofluorophosphate and sodium fluoride, cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, decalinium chloride, chlorhexidine hydrochloride,
Fungicides such as chlorhexidine gluconate, triclosan, isopropylmethylphenol, hinokitiol, sodium chloride, copper gluconate, sodium polyphosphate,
Inorganic salts and organic salts such as sodium metaphosphate, sodium orthophosphate, sodium tripolyphosphate, aluminum lactate and chitosan.

Examples of the surfactant include water-soluble salts of higher alkyl sulfates having 8 to 18 carbon atoms in the alkyl group, such as sodium lauryl sulfate and sodium myristyl sulfate, sodium lauryl monoglyceride sulfonate, coconut monoglyceride sulfonate. In addition to water-soluble salts of higher fatty acid monoglyceridesulfonic acid having 10 to 18 carbon atoms in the fatty acid group such as sodium, anionic surfactants such as olefinsulfonic acid and paraffinsulfonic acid, sucrose fatty acid esters, polyoxyethylene Nonionic surfactants such as hydrogenated castor oil, polyglycerin fatty acid esters, alkyl glycosides, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, alkyldimethylamine oxide, and alkyl Acid betaine, fatty acid amide propyl betaine type amphoteric surfactants such as betaine, N- fatty acyl -N
Imidazoline-type amphoteric surfactants such as -carboxymethyl-N-hydroxyethylethylenediamine salt.

Still other common components include, for example, saccharin sodium, stevioside, neohesperidyl dihydrochalcone, perillartin, thaumatin, salicylic acid, sodium salicylate, asparatyl phenylalanine methyl ester, p-methoxycinnamic aldehyde, sucrose, fructose, saccharamine Sweeteners such as sodium acid, spearmint oil, peppermint oil, wintergreen oil, sassafras oil, clove oil, eucalyptus oil, sage oil, mayonnaise oil, thyme oil, lemon oil, orange oil, l-menthol, carvone, anethole, salicylic acid Perfumes such as methyl, water-soluble polymers such as polyvinyl alcohol and polyvinyl pyrrolidone, sorbit, glycerin, ethylene glycol, propylene glycol as a thickener or wetting agent 1,3-butylene glycol, polyethylene glycol, polypropylene glycol, maltitol, Rakuchitto and the like.

[0017]

EFFECT OF THE INVENTION The oral liquid preparation containing xylitol of the present invention has a remarkably reduced bitterness during use and after use, and is excellent in use feeling.

[0018]

EXAMPLES The present invention will be described in more detail with reference to experimental examples and examples, but the present invention is not limited to these examples.

[Experimental Example] An oral liquid preparation was prepared in the usual manner using the components shown in Table 1, and the mouth liquid was rinsed by a specialized panelist for 30 seconds using this oral liquid preparation, and the aftertaste after thoroughly rinsing with water. The sensory evaluation was performed according to the following evaluation criteria. Table 1 shows the results. Palatability rating ：: There was no bitterness peculiar to xylitol, and there was a very good refreshing feeling. ：: The bitterness peculiar to xylitol was suppressed, and there was a good refreshing feeling. X: Strong bitterness peculiar to xylitol was present, and the refreshing feeling was insufficient.

[0020]

[Table 1] 1) Grapefruit oil: A solution obtained by dissolving an oil component in a hydroalcoholic solvent was used. Table 1 shows the actual oil component content. In the following Examples 1 and later, oil content was also indicated. 2) Pepper extract: Shown by solid content. Ethanol solvent extract. In the following Examples 1 and thereafter, the solid content was also shown.

[Example 1] (Mouthwash, using a transparent green PET container) Xylitol 5% by weight Ethanol 10 Grapefruit oil 0.005 Pepper extract (Ethanol extract) 0.004 Polyoxyethylene (EO60) hydrogenated castor oil 1.0 Citric acid 0.03 Sodium citrate 0.25 Fragrance 0.2 (Citrus system: l-menthol, cineol main compound) Sodium benzoate 0.3 Paraben 0.1 Purified water Balance meter 100% by weight

[Example 2] (Mouthwash, use of PET transparent green container) Xylitol 10% by weight Ethanol 7 Grapefruit oil 0.001 Pepper extract (ethanol extract) 0.002 Polyoxyethylene (EO40) hydrogenated castor oil 0.8 Malic acid 0.01 Sodium malate 0.1 Fragrance 0.3 (citrus system: 1-menthol, limonene main compound) Sodium benzoate 0.2 Paraben 0.1 Purified water Balance meter 100% by weight

[Example 3] (Mouthwash, using a transparent green PET container) Xylitol 20% by weight Ethanol 5 Grapefruit oil 0.003 Polyoxyethylene (EO60) hydrogenated castor oil 0.6 Tartaric acid 0.01 Sodium tartrate 0 0.3 Perfume 0.4 Sodium benzoate 0.1 Paraben 0.1 Purified water Balance meter 100% by weight

[Example 4] (Mouth washes, using a transparent green PET container) Xylitol 8% by weight Ethanol 13 Pepper extract (Ethanol extract) 0.006 Polyoxyethylene hydrogenated castor oil 1.5 Disodium hydrogen phosphate 0.4 Sodium dihydrogen phosphate 0.1 Perfume 0.2 Sodium benzoate 0.3 Paraben 0.1 Purified water Balance meter 100% by weight

Example 5 (Mouth washes, using a transparent green PET container) Xylitol 6% by weight Ethanol 11 Pepper extract (Ethanol extract) 0.05 Grapefruit oil 0.005 Polyoxyethylene (EO60) hydrogenated castor oil 1.3 Sodium fluoride 0.21 Citric acid 0.03 Sodium citrate 0.25 Fragrance 0.2 Sodium benzoate 0.3 Paraben 0.1 Purified water Balance meter 100% by weight

[Example 6] (Mouthwash, using a transparent PET container made of PET) Xylitol 15% by weight Ethanol 9 Pepper extract (Ethanol extract) 0.01 Tranexamic acid 0.01 Polyoxyethylene (EO60) hydrogenated castor oil 0.7 Rosemary extract 0.01 Malic acid 0.01 Sodium malate 0.1 Fragrance 0.3 Sodium benzoate 0.2 Paraben 0.1 Purified water Balance meter 100% by weight

[Example 7] (Mouthwash, using a transparent green PET container) Xylitol 18% by weight Ethanol 10 Grapefruit oil 0.001 Polyoxyethylene (EO60) hydrogenated castor oil 1.5 Sodium metaphosphate 0.4 Tartaric acid 0.01 Sodium tartrate 0.3 Perfume 0.4 Sodium benzoate 0.1 Paraben 0.1 Purified water Balance meter 100% by weight

[Example 8] (Mouthwash, using a transparent green PET container) Xylitol 20% by weight Ethanol 9 Pepper extract (ethanol extract) 0.004 Cetylpyridinium chloride 0.01 Polyoxyethylene (EO60) cured castor Oil 1.8 Disodium hydrogen phosphate 0.4 Sodium dihydrogen phosphate 0.1 Fragrance 0.2 Sodium benzoate 0.3 Paraben 0.1 Purified water Balance meter 100% by weight

Claims (2)

[Claims] 1. Xylitol and 2 to 20 parts of the total composition
An oral liquid preparation containing ethanol by weight and a bitterness regulator. 2. The oral liquid preparation according to claim 1, wherein the bitterness regulator is grapefruit oil, pepper extract or a mixture thereof.